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Reversible and irreversible binding of beta-funaltrexamine to mu, delta and kappa opioid receptors in guinea pig brain membranes.
J Pharmacol Exp Ther. 1986 Nov; 239(2):351-7.JP

Abstract

The effect of beta-funaltrexamine (beta-FNA), an irreversible mu receptor blocker in isolated tissue bioassays, on mu, kappa and delta opioid receptor binding and the binding of beta-[3H]FNA were determined in guinea pig brain membranes. beta-FNA inhibited the binding of mu, kappa and delta opioid ligands to their receptors with Ki values of 2.2, 14 and 78 nM, respectively. Pretreatment of brain membranes with beta-FNA (less than 2 microM) followed by extensive washing inhibited mu binding and to a lesser degree delta binding, without changing kappa binding. The extent of the irreversible inhibition was dependent on the concentration of beta-FNA, and this inhibition on mu binding could be observed with as little as 1 nM beta-FNA. The irreversible inhibition of mu binding by beta-FNA pretreatment was due to a decrease in the number of binding sites with little change in Kd, and was more pronounced in the presence of increasing concentrations of NaCl. Specific binding of beta-[3H]FNA to opioid receptors was demonstrated. The rate of specific binding with 2 nM beta-[3H]FNA was rapid in the initial 10 min and did not reach maximum in 90 min. The dissociation of bound beta-[3H]FNA (5 nM added) by the addition of excess unlabeled naloxone reached maximum at 30 min with approximately 35% of specifically bound beta-[3H]FNA remaining. Mu opioids were most effective in preventing specific binding of beta-[3H]FNA when added before beta-[3H]FNA. Opioids added 1 hr after 2 nM beta-[3H]FNA could displace maximally only 70 to 75% of specific binding.(ABSTRACT TRUNCATED AT 250 WORDS)

Authors

No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

3021954

Citation

Tam, S W., and L Y. Liu-Chen. "Reversible and Irreversible Binding of Beta-funaltrexamine to Mu, Delta and Kappa Opioid Receptors in Guinea Pig Brain Membranes." The Journal of Pharmacology and Experimental Therapeutics, vol. 239, no. 2, 1986, pp. 351-7.
Tam SW, Liu-Chen LY. Reversible and irreversible binding of beta-funaltrexamine to mu, delta and kappa opioid receptors in guinea pig brain membranes. J Pharmacol Exp Ther. 1986;239(2):351-7.
Tam, S. W., & Liu-Chen, L. Y. (1986). Reversible and irreversible binding of beta-funaltrexamine to mu, delta and kappa opioid receptors in guinea pig brain membranes. The Journal of Pharmacology and Experimental Therapeutics, 239(2), 351-7.
Tam SW, Liu-Chen LY. Reversible and Irreversible Binding of Beta-funaltrexamine to Mu, Delta and Kappa Opioid Receptors in Guinea Pig Brain Membranes. J Pharmacol Exp Ther. 1986;239(2):351-7. PubMed PMID: 3021954.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Reversible and irreversible binding of beta-funaltrexamine to mu, delta and kappa opioid receptors in guinea pig brain membranes. AU - Tam,S W, AU - Liu-Chen,L Y, PY - 1986/11/1/pubmed PY - 1986/11/1/medline PY - 1986/11/1/entrez SP - 351 EP - 7 JF - The Journal of pharmacology and experimental therapeutics JO - J Pharmacol Exp Ther VL - 239 IS - 2 N2 - The effect of beta-funaltrexamine (beta-FNA), an irreversible mu receptor blocker in isolated tissue bioassays, on mu, kappa and delta opioid receptor binding and the binding of beta-[3H]FNA were determined in guinea pig brain membranes. beta-FNA inhibited the binding of mu, kappa and delta opioid ligands to their receptors with Ki values of 2.2, 14 and 78 nM, respectively. Pretreatment of brain membranes with beta-FNA (less than 2 microM) followed by extensive washing inhibited mu binding and to a lesser degree delta binding, without changing kappa binding. The extent of the irreversible inhibition was dependent on the concentration of beta-FNA, and this inhibition on mu binding could be observed with as little as 1 nM beta-FNA. The irreversible inhibition of mu binding by beta-FNA pretreatment was due to a decrease in the number of binding sites with little change in Kd, and was more pronounced in the presence of increasing concentrations of NaCl. Specific binding of beta-[3H]FNA to opioid receptors was demonstrated. The rate of specific binding with 2 nM beta-[3H]FNA was rapid in the initial 10 min and did not reach maximum in 90 min. The dissociation of bound beta-[3H]FNA (5 nM added) by the addition of excess unlabeled naloxone reached maximum at 30 min with approximately 35% of specifically bound beta-[3H]FNA remaining. Mu opioids were most effective in preventing specific binding of beta-[3H]FNA when added before beta-[3H]FNA. Opioids added 1 hr after 2 nM beta-[3H]FNA could displace maximally only 70 to 75% of specific binding.(ABSTRACT TRUNCATED AT 250 WORDS) SN - 0022-3565 UR - https://www.unboundmedicine.com/medline/citation/3021954/Reversible_and_irreversible_binding_of_beta_funaltrexamine_to_mu_delta_and_kappa_opioid_receptors_in_guinea_pig_brain_membranes_ L2 - https://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=3021954 DB - PRIME DP - Unbound Medicine ER -